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Assay Detail

CHEMBL5224065

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of LSD1 (unknown origin)
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysine-specific histone demethylase 1A (CHEMBL6136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021.
Song Y, Zhang H, Yang X, Shi Y, Yu B.
Eur J Med Chem (2022) 228 : 114042 -114042
PubMed 34915312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.47 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775474 1 8.54
CHEMBL4749146 1 8.30
CHEMBL5268105 1 7.96
CHEMBL4857832 1 7.96
CHEMBL4860694 1 7.77
CHEMBL5276713 1 7.66
CHEMBL5286191 1 7.54
CHEMBL4854446 1 7.28
CHEMBL5290883 1 7.21
CHEMBL5182796 1 7.20
CHEMBL4863608 1 7.19
CHEMBL4862640 1 6.87
CHEMBL5201233 1 6.85
CHEMBL5204771 1 6.72
CHEMBL4436792 1 6.55
CHEMBL5283767 1 6.52
CHEMBL5284828 1 6.40
CHEMBL5282096 1 6.34
CHEMBL4868123 1 6.16
CHEMBL5280652 1 6.16
CHEMBL5270361 1 6.09
CHEMBL4864525 1 6.09
CHEMBL5272643 1 6.05
CHEMBL588 FENOLDOPAM 4.0 1 6.05
CHEMBL5075646 1 6.03
CHEMBL5286264 1 5.99
CHEMBL5274410 1 5.90
CHEMBL19344 HIGENAMINE 1.0 1 5.83
CHEMBL5093633 1 5.79
CHEMBL4871961 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775474 IC50 = 2.9 nM 8.54
CHEMBL4749146 IC50 = 5.0 nM 8.30
CHEMBL4857832 IC50 = 11.0 nM 7.96
CHEMBL5268105 IC50 = 11.0 nM 7.96
CHEMBL4860694 IC50 = 17.0 nM 7.77
CHEMBL5276713 IC50 = 22.0 nM 7.66
CHEMBL5286191 IC50 = 29.0 nM 7.54
CHEMBL4854446 IC50 = 53.0 nM 7.28
CHEMBL5290883 IC50 = 61.0 nM 7.21
CHEMBL5182796 IC50 = 63.0 nM 7.20
CHEMBL4863608 IC50 = 65.0 nM 7.19
CHEMBL4862640 IC50 = 135.0 nM 6.87
CHEMBL5201233 IC50 = 140.0 nM 6.85
CHEMBL5204771 IC50 = 190.0 nM 6.72
CHEMBL4436792 IC50 = 283.0 nM 6.55
CHEMBL5283767 IC50 = 300.0 nM 6.52
CHEMBL5284828 IC50 = 400.0 nM 6.40
CHEMBL5282096 IC50 = 460.0 nM 6.34
CHEMBL4868123 IC50 = 690.0 nM 6.16
CHEMBL5280652 IC50 = 700.0 nM 6.16
CHEMBL5270361 IC50 = 820.0 nM 6.09
CHEMBL4864525 IC50 = 810.0 nM 6.09
CHEMBL5272643 IC50 = 890.0 nM 6.05
CHEMBL588 FENOLDOPAM IC50 = 890.0 nM 6.05
CHEMBL5075646 IC50 = 930.0 nM 6.03
CHEMBL5286264 IC50 = 1020.0 nM 5.99
CHEMBL5274410 IC50 = 1250.0 nM 5.90
CHEMBL19344 HIGENAMINE IC50 = 1470.0 nM 5.83
CHEMBL5093633 IC50 = 1640.0 nM 5.79
CHEMBL4871961 IC50 = 1890.0 nM 5.72
CHEMBL2334501 IC50 = 2100.0 nM 5.68
CHEMBL81 RALOXIFENE IC50 = 2080.0 nM 5.68
CHEMBL5280719 IC50 = 2330.0 nM 5.63
CHEMBL4066708 IC50 = 2900.0 nM 5.54
CHEMBL5084881 IC50 = 3550.0 nM 5.45
CHEMBL5281624 IC50 = 4810.0 nM 5.32
CHEMBL2046709 IC50 = 4880.0 nM 5.31
CHEMBL553 ERLOTINIB IC50 = 35800.0 nM 4.45
CHEMBL3759201 IC50 = 134000.0 nM -
CHEMBL4742730 IC50 = 540.0 nM -